Lopinavir

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Lopinavir
Lopinavir.svg
Lopinavir ball-and-stick.png
Systematic (IUPAC) name
(2S)-N-[(2S,4S,5S)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
Clinical data
AHFS/Drugs.com International Drug Names
MedlinePlus a602015
Pregnancy cat. C (US)
Legal status POM (UK) -only (US)
Routes Oral
Pharmacokinetic data
Bioavailability Unknown
Protein binding 98-99%
Metabolism Hepatic
Half-life 5 to 6 hours
Excretion Mostly fecal
Identifiers
CAS number 192725-17-0 YesY
ATC code J05AR10 (with ritonavir)
PubChem CID 92727
DrugBank DB01601
ChemSpider 83706 YesY
UNII 2494G1JF75 YesY
KEGG D01425 YesY
ChEMBL CHEMBL729 YesY
Chemical data
Formula C37H48N4O5 
Mol. mass 628.810 g/mol
 YesY (what is this?)  (verify)

Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir, under the trade names Kaletra (high-income countries) and Aluvia (low-income countries). It was first approved by the FDA on 15 September 2000.[1]

Pharmacology[edit]

Lopinavir is highly bound to plasma proteins (98–99%).[2]

Reports are contradictory regarding lopinavir penetration into the cerebrospinal fluid (CSF). Anecdotal reports state that lopinavir cannot be detected in the CSF; however, a study of paired CSF-plasma samples from 26 patients receiving lopinavir/ritonavir found lopinavir CSF levels above the IC50 in 77% of samples.[3]

Clinical properties[edit]

Side effects, interactions, and contraindications have only been evaluated in the drug combination lopinavir/ritonavir.

Research[edit]

A 2014 study indicates that lopinavir is effective against the human papilloma virus (HPV). The study used the equivalent of one tablet twice a day applied topically to the cervices of women with high-grade and low-grade precancerous conditions. After three months of treatment, 82.6% of the women who had high-grade disease had normal cervical conditions, confirmed by smears and biopsies.[4]

References[edit]

  1. ^ "FDA Approved Drug Products: Kaletra". Retrieved 30 April 2004. 
  2. ^ KALETRA (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
  3. ^ Capparelli E, Holland D, Okamoto C, et al. (2005). "Lopinavir concentrations in cerebrospinal fluid exceed the 50% inhibitory concentration for HIV". AIDS (London, England) 19 (9). 
  4. ^ HIV drug used to reverse effects of virus that causes cervical cancer University of Manchester, 17 February 2014.

External links[edit]